Many pathological states caused by deficiencies in or complete failure of the production of certain macromolecules (e.g. proteins and peptides) are treated with an invasive and inconvenient parenteral administration of therapeutic macromolecules. One example hereof is administration of GLP-1 in the treatment of type 2 diabetes.
The oral route is desirable for administration due to its non-invasive nature and has a great potential to decrease the patient's discomfort related to administration of a drug substance and to increase patient compliance with administration of a drug substance. However, several problems exist; such as the enzymatic degradation in the gastrointestinal tract and limited permeability over the gastrointestinal membrane leading to insufficient and variable absorption. At present no products for oral delivery of GLP-1 agonists have been marketed.
Provision of a solid oral dosage form which would facilitate oral administration of GLP-1 is desirable. The advantages of solid oral dosage forms over other dosage forms include ease of manufacture, storage and administration. There may also be advantages relating to convenience of administration increasing patient compliance.
However, oral administration of GLP-1 agonists is challenged by poor bioavailability of GLP-1 agonists. Thus, new compositions providing improved oral bioavailability of GLP-1 agonists are desired.